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pentamidine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
	2090	100-33-4

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: pentamidine isetionate pentamidine diisethionate pentamidine pentamidine isethionate pentamidin pentamidine mesylate pentamidine mesilate	Antiprotozoal agent effective in trypanosomiasis, leishmaniasis, and some fungal infections; used in treatment of PNEUMOCYSTIS pneumonia in HIV-infected patients. It may cause diabetes mellitus, central nervous system damage, and other toxic effects. Molecular weight: 340.43 Formula: C19H24N4O2 CLOGP: 2.31 LIPINSKI: 0 HAC: 6 HDO: 4 TPSA: 118.20 ALOGS: -4.16 ROTB: 10 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

pentamidine isetionate
pentamidine diisethionate
pentamidine
pentamidine isethionate
pentamidin
pentamidine mesylate
pentamidine mesilate

Antiprotozoal agent effective in trypanosomiasis, leishmaniasis, and some fungal infections; used in treatment of PNEUMOCYSTIS pneumonia in HIV-infected patients. It may cause diabetes mellitus, central nervous system damage, and other toxic effects.

Molecular weight: 340.43
Formula: C19H24N4O2
CLOGP: 2.31
LIPINSKI: 0
HAC: 6
HDO: 4
TPSA: 118.20
ALOGS: -4.16
ROTB: 10

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
0.28	g	P

ADMET properties:

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Property	Value	Reference
CL (Clearance)	74 mL/min/kg	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	53 L/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	25 hours	Lombardo F, Berellini G, Obach RS
EoM (Fraction excreted unchanged in urine)	12 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	11.75 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
S (Water solubility)	100 mg/mL	Benet LZ, Broccatelli F, Oprea TI
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.09 %	Lombardo F, Berellini G, Obach RS
BA (Bioavailability)	0 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

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Approvals:

Date	Agency	Company	Orphan
Oct. 16, 1984	FDA	FRESENIUS KABI USA

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Aplastic anaemia	162.39	24.07	51	5210	9518	63474243
Febrile neutropenia	147.42	24.07	102	5159	118347	63365414
Pneumocystis jirovecii pneumonia	126.78	24.07	49	5212	16865	63466896
Toxoplasmosis	123.46	24.07	28	5233	1495	63482266
Nocardiosis	81.14	24.07	21	5240	1955	63481806
Antinuclear antibody negative	71.64	24.07	13	5248	221	63483540
Hypoalbuminaemia	66.97	24.07	28	5233	11777	63471984
Coombs positive haemolytic anaemia	65.66	24.07	13	5248	358	63483403
Cytomegalovirus viraemia	63.22	24.07	22	5239	5627	63478134
Antithrombin III	62.49	24.07	11	5250	156	63483605

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Nocardiosis	169.68	20.19	53	7102	3898	34945878
Aplastic anaemia	110.16	20.19	49	7106	9667	34940109
Toxoplasmosis	102.35	20.19	28	7127	1288	34948488
Mucosal inflammation	97.48	20.19	73	7082	38549	34911227
Febrile bone marrow aplasia	94.98	20.19	42	7113	8167	34941609
Cerebral toxoplasmosis	94.92	20.19	28	7127	1693	34948083
Pneumocystis jirovecii pneumonia	62.90	20.19	43	7112	19667	34930109
Febrile neutropenia	62.17	20.19	105	7050	136744	34813032
Respiratory failure	61.27	20.19	92	7063	108480	34841296
Troponin T increased	58.63	20.19	21	7134	2350	34947426

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Aplastic anaemia	262.58	19.03	98	11255	17807	79715228
Nocardiosis	256.76	19.03	73	11280	5606	79727429
Toxoplasmosis	203.74	19.03	52	11301	2645	79730390
Febrile neutropenia	195.18	19.03	200	11153	230799	79502236
Pneumocystis jirovecii pneumonia	141.55	19.03	76	11277	32432	79700603
Respiratory failure	101.84	19.03	127	11226	180784	79552251
Neutropenia	100.98	19.03	161	11192	287549	79445486
Cerebral toxoplasmosis	100.63	19.03	29	11324	2333	79730702
Mucosal inflammation	99.62	19.03	84	11269	75496	79657539
Cytokine release syndrome	95.35	19.03	61	11292	35937	79697098

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	P01CX01	ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS ANTIPROTOZOALS AGENTS AGAINST LEISHMANIASIS AND TRYPANOSOMIASIS Other agents against leishmaniasis and trypanosomiasis
CHEBI has role	CHEBI:36335	trypanocidal drugs
CHEBI has role	CHEBI:35703	Xenobiotic
CHEBI has role	CHEBI:35718	antifungal agents
CHEBI has role	CHEBI:60643	N-methyl-D-aspartate receptor antagonists
CHEBI has role	CHEBI:63673	CCR5 antagonist
CHEBI has role	CHEBI:67079	anti-inflammatory agents
CHEBI has role	CHEBI:76395	histone acetyltransferase inhibitors
CHEBI has role	CHEBI:136651	S100 calcium-binding protein B inhibitors
FDA EPC	N0000175485	Antiprotozoal

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
African trypanosomiasis	indication	27031003	DOID:10112
Pneumocystosis jiroveci pneumonia	indication	415125002	DOID:11339
Pneumocystis Carinii Pneumonia Prevention	indication
Visceral leishmaniasis	off-label use	186803007	DOID:9146
Cutaneous leishmaniasis	off-label use	240637006	DOID:9111
Hypocalcemia	contraindication	5291005
Hyperkalemia	contraindication	14140009
Torsades de pointes	contraindication	31722008
Dehydration	contraindication	34095006
Hypertensive disorder	contraindication	38341003	DOID:10763

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	11.38	Basic
pKa2	10.78	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Type	Activity value (-log[M])	Bioact source
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN	Ki	6.29	DRUG MATRIX
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN	Ki	4.89	DRUG MATRIX
Sodium-dependent noradrenaline transporter	Transporter	P23975	SC6A2_HUMAN	Ki	5.66	DRUG MATRIX
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN	Ki	6.33	DRUG MATRIX
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN	Ki	5.77	DRUG MATRIX
D(3) dopamine receptor	GPCR	P35462	DRD3_HUMAN	Ki	5.87	DRUG MATRIX
Muscarinic acetylcholine receptor M2	GPCR	P08172	ACM2_HUMAN	Ki	6.30	DRUG MATRIX
Muscarinic acetylcholine receptor M4	GPCR	P08173	ACM4_HUMAN	Ki	6.66	DRUG MATRIX
Muscarinic acetylcholine receptor M5	GPCR	P08912	ACM5_HUMAN	Ki	5.68	DRUG MATRIX
Sodium-dependent dopamine transporter	Transporter	Q01959	SC6A3_HUMAN	Ki	5.60	DRUG MATRIX

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External reference:

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ID	Source
002971	NDDF
140-64-7	SECONDARY_CAS_RN
16826009	SNOMEDCT_US
2196	MMSL
31692006	SNOMEDCT_US
372699006	SNOMEDCT_US
4019043	VUID
4019043	VANDF
4019881	VANDF
4167	INN_ID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
NebuPent	Human Prescription Drug Label	1	63323-877	INHALANT	300 mg	RESPIRATORY (INHALATION)	NDA	12 sections
Pentam 300	HUMAN PRESCRIPTION DRUG LABEL	1	63323-113	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	300 mg	INTRAMUSCULAR	NDA	13 sections
Pentam 300	HUMAN PRESCRIPTION DRUG LABEL	1	63323-113	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	300 mg	INTRAMUSCULAR	NDA	13 sections
Pentamidine Isethionate	HUMAN PRESCRIPTION DRUG LABEL	1	13925-515	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	300 mg	INTRAMUSCULAR	ANDA	13 sections
Pentamidine Isethionate	HUMAN PRESCRIPTION DRUG LABEL	1	13925-515	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	300 mg	INTRAMUSCULAR	ANDA	13 sections
Pentamidine Isethionate	HUMAN PRESCRIPTION DRUG LABEL	1	13925-522	INHALANT	300 mg	RESPIRATORY (INHALATION)	ANDA	21 sections
Pentamidine Isethionate	HUMAN PRESCRIPTION DRUG LABEL	1	13925-522	INHALANT	300 mg	RESPIRATORY (INHALATION)	ANDA	21 sections
pentamidine isethionate	HUMAN PRESCRIPTION DRUG LABEL	1	23155-748	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	300 mg	INTRAMUSCULAR	ANDA	17 sections
Pentamidine Isethionate	HUMAN PRESCRIPTION DRUG LABEL	1	39822-3030	INHALANT	300 mg	RESPIRATORY (INHALATION)	ANDA	22 sections
PENTAMIDINE ISETHIONATE	HUMAN PRESCRIPTION DRUG LABEL	1	39822-3050	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	300 mg	INTRAVENOUS	ANDA	24 sections

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